8-Chloroadenosine

8-Chloroadenosine (NSC-354258) 是一种 5' AMP 激活的蛋白激酶激动剂,可能用于治疗慢性淋巴细胞白血病。 它的活性与 mTOR 通路的抑制有关。它是一种核苷类似物。在体内代谢为 8-氯-ATP。在转录过程中掺入 RNA 并抑制 RNA 合成。在 MM.1S、RPMI-8226 和 U266 癌细胞系中表现出细胞毒性;在 A549 和 H1299 细胞中诱导 G2/M 细胞周期停滞和有丝分裂灾难。它已被证明可消耗 ATP 并抑制血液恶性肿瘤以及肺癌和乳腺癌细胞系中的肿瘤生长。

CAS号

34408-14-5

分子式

C10H12ClN5O4

主要靶点

AMPK

仅限科研使用

Cat No : CM12580

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Synonyms

8-氯腺嘌呤核苷|8-Cl-Ado|NSC 354258|NSC354258|NSC-354258



产品信息

8-Chloroadenosine is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia. 8-chloroadenosine activity is associated with inhibition of the mTOR pathway.8-Chloroadenosine is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP. Incorporates into RNA during transcription and inhibits RNA synthesis. Exhibits cytotoxicity in MM.1S, RPMI-8226, and U266 cancer cell lines; induces G2/M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. 8-Chloroadenosine has been shown to deplete ATP and inhibit tumor growth in hematological malignancies as well as in lung and breast cancer cell lines.

CAS号 34408-14-5
分子式 C10H12ClN5O4
主要靶点 AMPK
主要通路 表观遗传|PI3K/Akt/mTOR信号通路
分子量 301.69
纯度 99.48%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 8-氯腺嘌呤核苷|8-Cl-Ado|NSC 354258|NSC354258|NSC-354258

溶解度

DMSO:65 mg/ml (215.45 mM)

参考文献

1.Dicitore A, Grassi ES, Caraglia M, Borghi MO, Gaudenzi G, Hofland LJ, Persani L, Vitale G. The cAMP analogs have potent anti-proliferative effects on medullary thyroid cancer cell lines. Endocrine. 2016 Jan;51(1):101-12. doi: 10.1007/s12020-015-0597-7. PubMed PMID: 25863490.
2.Zhang et al (2004) Exposure of human lung cancer cells to 8-chloro-adenosine induces G2/M arrest and mitotic catastrophe. Neoplasia 6 802 PMID: 15720807
3.Stellrecht CM, Vangapandu HV, Le XF, Mao W, Shentu S. ATP directed agent, 8-chloro-adenosine, induces AMP activated protein kinase activity, leading to autophagic cell death in breast cancer cells. J Hematol Oncol. 2014 Mar 14;7:23. doi: 10.1186/1756-8722-7-23. PubMed PMID: 24628795; PubMed Central PMCID: PMC4007639.
4.Han YY, Zhou Z, Cao JX, Jin YQ, Li SY, Ni JH, An GS, Zhang YX, Jia HT. E2F1-mediated DNA damage is implicated in 8-Cl-adenosine-induced chromosome missegregation and apoptosis in human lung cancer H1299 cells. Mol Cell Biochem. 2013 Dec;384(1-2):187-96. doi: 10.1007/s11010-013-1797-1. PubMed PMID: 24037421.

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